Results 261 to 270 of about 42,993 (314)

Design and synthesis of a fluorescent muscarinic antagonist

Bioorganic & Medicinal Chemistry Letters, 2008
The design and concise synthesis of a fluorescent tolterodine-BODIPY (boron dipyrromethene) conjugate is described which possesses potent antimuscarinic activity. This derivative illustrates proof-of-concept for the preparation of other useful fluorophoric antimuscarinic agents which have potential utility in receptor occupancy studies and high ...
Lyn H, Jones, Amy, Randall, Carolyn, Napier, Mike, Trevethick, Sasha, Sreckovic, Jessica, Watson   +5 more
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Binding of agonists and antagonists to muscarinic receptors

Journal of Supramolecular Structure, 1976
AbstractThe binding of one irreversible and two reversible radioactive antagonists to muscarinic receptors in synaptosome preparations of rat cerebral cortex has been studied. The ligands all bind to the same receptor pool and directly and competitively yield self‐consistent binding constants closely similar to those obtained by pharmacological methods
N J, Birdsall, A S, Burgen, C R, Hiley, E C, Hulme   +3 more
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Allosteric antagonists of the muscarinic acetylcholine receptor

Biochemical Pharmacology, 1991
For the most part, the interaction of these selective antagonists with muscarinic receptors has been interpreted in the context of simple competitive bimolecular reaction which obeys the law of mass action. In fact, the use of selective antagonists as a pharmacological tool to identify receptor types and subtypes is based on this premise.
N H, Lee, E E, el-Fakahany
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MUSCARINIC RECEPTOR ANTAGONISTS

1991
A muscarinic receptor antagonist of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is N or (a) where R is H, halo or C1-C4 alkyl; R is H or C1-C4 alkyl; R is H or C1-C4 alkyl; Y is a direct link, O or S; m is an integer of from 1 to 4; n is 2 or 3; and R is 1- or 2-naphthyl or a group of formula (b), (c) or Het where R and R are ...
PFIZER LTD, PFIZER
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Aprophit: An irreversible antagonist for muscarinic receptors

Biochemical Pharmacology, 1990
The development of selective irreversible ligands has proven to be an invaluable technique for the isolation, purification and characterization of many receptor proteins. An isothiocyanato-derivative of the muscarinic antagonist aprophen was synthesized and evaluated as a potential irreversible ligand for muscarinic receptors.
A H, Newman, J, Covington, M, Oleshansky, B W, Jackson, B A, Weissman, H, Leader, P K, Chiang   +6 more
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[Selective muscarinic receptor antagonists].

Nihon rinsho. Japanese journal of clinical medicine, 1984
to ex- plain the anomalous binding of cholin- ergic agonists to brain receptors~ were later demonstrated with the seEective muscarinic antagonist, pirenzepine 2. Interestingly, the search for selective antagonists, which usually follows the acceptance of a concept, antedated by many years the notion of heterogeneity of rmecarinic receptors. Intuitively
S, Kishimoto, G, Kajiyama, A, Miyoshi
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Muscarinic receptor antagonists for overactive bladder

BJU International, 2007
From time to time we publish a full review of drugs that are available for the treatment of common conditions. In this issue, the review is written by two of the leading authorities in the world, Paul Abrams and Karl‐Erik Andersson, on the topic of overactive bladder and antimuscarinic agents.
Paul, Abrams, Karl-Erik, Andersson
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Muscarinic receptor agonists and antagonists

Expert Opinion on Therapeutic Patents, 1999
Although four different subtypes of the muscarinic acetylcholine (ACh) receptor with functional correlates are known to exist (function for M5 is still unclear), all muscarinic agonists and antagon...
Darius P Zlotos, Wiebke Bender, Ulrike Holzgrabe   +2 more
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Muscarinic autoreceptors are differentially affected by selective muscarinic antagonists in rat hippocampus

Neurochemistry International, 1989
The effects of atropine, pirenzepine and AF-DX 116 on the high K(+)-evoked release of endogenous ACh from rat hippocampal slices were compared. As expected, atropine in concentrations of 10(?5) and 10(?6)M increased the release of acetylcholine, to 128 and 157% of the control value, respectively. While AF-DX 116 was also able to increase the release to
K, Gulya, D, Budai, P, Kása
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The discovery of AZD9164, a novel muscarinic M3 antagonist

Bioorganic & Medicinal Chemistry Letters, 2011
The optimization of a new series of muscarinic M(3) antagonists is described, leading to the identification of AZD9164 which was progressed into the clinic for evaluation of its potential as a treatment for COPD.
Antonio, Mete, Keith, Bowers, Eric, Chevalier, David K, Donald, Helen, Edwards, Katherine J, Escott, Rhonan, Ford, Ken, Grime, Ian, Millichip, Barry, Teobald, Vince, Russell   +10 more
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